Target Information

Target General Infomation
Target ID
T99524
Former ID
TTDI01906
Target Name
Trace amine-associated receptor-1
Gene Name
TAAR1
Synonyms
TaR-1; Trace amine receptor 1; TAAR1
Target Type
Successful
Disease Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Attention deficit disorder with hyperactivity [ICD10: F90]
Attention deficit hyperactivity disorder; Narcolepsy [ICD10: F90, G47.4]
Diagnostic evaluation of horner's syndrome [ICD10: G90.2]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Unspecified [ICD code not available]
Function
Receptor for trace amines, including beta- phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amines,such as epinephrine and histamine and only partially activated by dopamine and serotonine. Trace amines are biogenic amines present in very low levels in mammalian tissues. Although some trace amineshave clearly defined roles as neurotransmitters in invertebrates, the extent to which they function as true neurotransmitters in vertebrates has remained speculative. Trace amines are likely to be involved in a variety of physiological functions that have yet to be fully understood. The signal transduced by this receptor is mediated by the G(s)-class of G-proteins which activate adenylate cyclase.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q96RJ0
Sequence
MMPFCHNIINISCVKNNWSNDVRASLYSLMVLIILTTLVGNLIVIVSISHFKQLHTPTNW
LIHSMATVDFLLGCLVMPYSMVRSAEHCWYFGEVFCKIHTSTDIMLSSASIFHLSFISID
RYYAVCDPLRYKAKMNILVICVMIFISWSVPAVFAFGMIFLELNFKGAEEIYYKHVHCRG
GCSVFFSKISGVLTFMTSFYIPGSIMLCVYYRIYLIAKEQARLISDANQKLQIGLEMKNG
ISQSKERKAVKTLGIVMGVFLICWCPFFICTVMDPFLHYIIPPTLNDVLIWFGYLNSTFN
PMVYAFFYPWFRKALKMMLFGKIFQKDSSRCKLFLELSS
Drugs and Mode of Action
Drug(s) Amphetamine Drug Info Approved Attention deficit disorder with hyperactivity [551871]
Dextroamphetamine Drug Info Approved Attention deficit hyperactivity disorder; Narcolepsy [551871]
Hydroxyamphetamine Hydrobromide Drug Info Approved Diagnostic evaluation of horner's syndrome [551871]
Lisdexamfetamine Drug Info Approved Attention deficit hyperactivity disorder [538579], [542228]
NT0202 Drug Info Phase 3 Attention deficit hyperactivity disorder [526471], [526676], [532175], [532852], [551871]
SPD-465 Drug Info Phase 3 Attention deficit hyperactivity disorder [526471], [526676], [532175], [532852], [551871]
D-amphetamine transdermal Drug Info Phase 2 Attention deficit hyperactivity disorder [526471], [526676], [532175], [532852], [551871]
RG-7351 Drug Info Phase 1 Major depressive disorder [549026]
Amphetamine Drug Info Investigative Attention deficit hyperactivity disorder [468035], [526471], [526676], [532175], [532852], [551871]
Agonist 3-iodothyronamine Drug Info [528833]
NT0202 Drug Info [526471], [526676], [532175], [532852], [551871]
R(-)amphetamine Drug Info [528610]
RG-7351 Drug Info [526471], [526676], [532175], [532852], [551610], [551871]
RO5166017 Drug Info [531452]
SPD-465 Drug Info [526471], [526676], [532175], [532852], [551871]
tyramine Drug Info [531694]
[3H]tyramine Drug Info [526105]
Modulator Amphetamine Drug Info [526471], [526676], [532175], [532852], [551871]
D-amphetamine transdermal Drug Info [526471], [526676], [532175], [532852], [551871]
Dextroamphetamine Drug Info [526471], [526676], [532175], [532852]
dextroamphetamine sulfate (oral liquid, ADHD), Auriga Drug Info [526471], [526676], [532175], [532852]
Hydroxyamphetamine Hydrobromide Drug Info
Lisdexamfetamine Drug Info [529282], [531678]
methamphetamine intravenous Drug Info [526471], [526676], [532175], [532852]
PF-08 Drug Info [526471], [526676], [532175], [532852], [551871]
Antagonist EPPTB Drug Info [530500]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome G alpha (s) signalling events
References
Ref 468035(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4804).
Ref 526471Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice. Neurosci Lett. 2002 Dec 16;334(3):145-8.
Ref 526676Alpha-1B adrenergic receptor knockout mice are protected against methamphetamine toxicity. J Neurochem. 2003 Jul;86(2):413-21.
Ref 532175Involvement of the alpha(1D)-adrenergic receptor in methamphetamine-induced hyperthermia and neurotoxicity in rats. Neurotox Res. 2013 Aug;24(2):130-8.
Ref 532852Methamphetamine and HIV-1-induced neurotoxicity: role of trace amine associated receptor 1 cAMP signaling in astrocytes. Neuropharmacology. 2014 Oct;85:499-507.
Ref 538579FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021977.
Ref 542228(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7213).
Ref 549026Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031597)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526105Trace amines: identification of a family of mammalian G protein-coupled receptors. Proc Natl Acad Sci U S A. 2001 Jul 31;98(16):8966-71. Epub 2001 Jul 17.
Ref 526471Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice. Neurosci Lett. 2002 Dec 16;334(3):145-8.
Ref 526676Alpha-1B adrenergic receptor knockout mice are protected against methamphetamine toxicity. J Neurochem. 2003 Jul;86(2):413-21.
Ref 528610The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia. Genes Brain Behav. 2007 Oct;6(7):628-39. Epub 2006 Dec 21.
Ref 528833Exploring the structure-activity relationship of the ethylamine portion of 3-iodothyronamine for rat and mouse trace amine-associated receptor 1. J Med Chem. 2007 Jun 14;50(12):2787-98. Epub 2007 May 12.
Ref 5292822007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
Ref 530500The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.
Ref 531452TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8485-90.
Ref 531678Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class. Bioorg Med Chem. 2011 Dec 1;19(23):7044-8.
Ref 531694Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists. PLoS One. 2011;6(10):e27073.
Ref 532175Involvement of the alpha(1D)-adrenergic receptor in methamphetamine-induced hyperthermia and neurotoxicity in rats. Neurotox Res. 2013 Aug;24(2):130-8.
Ref 532852Methamphetamine and HIV-1-induced neurotoxicity: role of trace amine associated receptor 1 cAMP signaling in astrocytes. Neuropharmacology. 2014 Oct;85:499-507.
Ref 551610Clinical pipeline report, company report or official report of Roche.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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